Assay Detail
Binding
CHEMBL993708
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]astemizole from human ERG expressed in HEK293 cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel approach for chemotype hopping based on annotated databases of chemically feasible fragments and a prospective case study: new melanin concentrating hormone antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.43 | 5.93 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214957 | — | — | 1 | 5.93 |
| CHEMBL470633 | — | — | 1 | 5.21 |
| CHEMBL470840 | — | — | 1 | 5.14 |
| CHEMBL512873 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214957 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL470633 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL470840 | — | IC50 | = | 7300.0 | nM | 5.14 |
| CHEMBL512873 | — | IC50 | - | — | - |